2055228-33-4

2055228-33-4 structure

2055228-33-4 structure

Name: SERT-IN-2
Chemical Name: SERT-IN-2
CAS Number: 2055228-33-4
Molecular Formula: C₂₆H₂₄F₂N₆
Molecular Weight: 458.51
Catalog: Signaling Pathways Neuronal Signaling Serotonin Transporter
Create Date: 2023-04-05 12:08:00
Modify Date: 2024-04-06 18:33:17
SERT-IN-2 is a potent SERT inhibitor (IC50=0.58 nM) with promising anti-depression efficacy. SERT-IN-2 shows good bioavailability of 83.28% in rats. SERT-IN-2 can cross the blood-brain barrier[1].

Name	SERT-IN-2

Description	SERT-IN-2 is a potent SERT inhibitor (IC50=0.58 nM) with promising anti-depression efficacy. SERT-IN-2 shows good bioavailability of 83.28% in rats. SERT-IN-2 can cross the blood-brain barrier[1].
Related Catalog	Research Areas >> Neurological Disease Signaling Pathways >> Neuronal Signaling >> Serotonin Transporter
Target	IC50: 0.58 nM (SERT)[1]
In Vivo	SERT-IN-2 (DH4) (2.5 mg/kg, 5 mg/kg; 口服或静脉注射; 单次剂量) 显示高血浆暴露和口服生物利用度在狗和大鼠[1]。 SERT-IN-2 (10 mg/kg; 腹腔注射; 单次剂量) 可以穿过 SD 大鼠的血脑屏障[1]。 SERT-IN-2 (1-10 mg/kg; 腹腔注射; 单次剂量) 抑制 5-羟色胺的摄取，并有效拮抗大鼠下丘脑中 p-chloroamphetamine (PCA) 诱导的 5-羟色胺的消耗[1]。 SERT-IN-2 (1-10 mg/kg; 静脉注射; 试验前给药 3 次) 对大鼠有抗抑郁作用，并呈剂量依赖性地减少强迫游泳试验 (FST) 的不动次数[1]。药代动力学分析[1] Route Dose (mg/kg) Cmax (ng/mL) AUC(0-t) (ng·h/mL) T1/2 (h) Vss (L/kg) Cl (L/h/kg) F (%) Rat IV 1 193 1340 7.53 6.41 11.6 / PO 2.5 180 2790 7.28 / / 83.28 Dog IV 1 520 2820 4.39 3.4 5.14 / PO 5 794 7540 16.4 / / 53.5
References	[1]. Wang ZZ, et al. Deciphering Nonbioavailable Substructures Improves the Bioavailability of Antidepressants by Serotonin Transporter. J Med Chem. 2023 Jan 12;66(1):371-383.

Molecular Formula	C₂₆H₂₄F₂N₆
Molecular Weight	458.51